The Influence of Water Content of Triglyceride Oils on the Solubility of Steroids

Abstract

Hydration of triglyceride oils caused a significant decrease in the solubility of steroids, which may form hydrates or hemihydrates. Results suggest the need for knowledge of the hydration state of triglyceride oils to be used as pharmaceutical excipients.

Mass Transport Properties of Progesterone and Estradiol in Model Microemulsion Formulations

“…The solubilities of each steroid in the 1ME and 0.5ME formulations were identical within experimental error. As confirmed previously, the progesterone was in the anhydrous form, while the estradiol was in the hemihydrate form (14). There was no evidence of polymorph change (14).…”

“…Solubilities of progesterone and estradiol in microemulsion formulations 3ME, 1ME and 0.5ME and in water were determined as outlined previously (14). The various formulations were exposed to excess solid progesterone or estradiol (Sigma Chemical) with an appropriate amount of 3 H-labeled drug in 4 ml glass vials with Teflon lined caps.…”

Olive Oil-Based Delivery of Photosensitizers for Bacterial Eradication

“…Colloid dispersions of solid triacylglycerol 140 nm-sized nanoparticles stabilized with poly(vinyl alcohol) were applied for delivery of the drugs diazepam and ubidecarenone (Rosenblat & Bunje, 2009). Soybean and olive oils were suggested as drug delivery vehicles for the steroids progesterone, estradiol and testosterone (Land et al, 2005). All of the abovementioned examples illustrate successful use of lipid-based systems for delivery of hydrophobic drugs.…”

Soft Gelatin Capsules (Softgels)

“…[252][253][254] The presence of water in a lipid vehicle may alter the solubility of a compound by one of three ways: (a) via disruption of hydrogen bonding between the molecules of the lipid and those of the solubilized compound and thereby reducing the solubility if this hydrogen bonding is a major driving force for the solubilization of the compound in the lipid; 252 (b) via inducing reorganization of the lipid molecules within the matrix from the original molecular arrangement existed in the absence of water; 254 and/or (c) via formation of a hydrate of the dissolved compound having reduced lipid solubility. [252][253][254] The presence of water in a lipid vehicle may alter the solubility of a compound by one of three ways: (a) via disruption of hydrogen bonding between the molecules of the lipid and those of the solubilized compound and thereby reducing the solubility if this hydrogen bonding is a major driving force for the solubilization of the compound in the lipid; 252 (b) via inducing reorganization of the lipid molecules within the matrix from the original molecular arrangement existed in the absence of water; 254 and/or (c) via formation of a hydrate of the dissolved compound having reduced lipid solubility.…”